- DERIVATIVES OF PIPERLONGUMINE AND USES THEREOF
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The present invention relates to a group of 1-[(E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]-2,3-dihydropyridin-6-one (piperlongumine) derivatives, analogs and pharmaceutically acceptable salts thereof. The present invention also relates to a pharmaceutical composition and formulation containing a derivative of piperlongumine; and use of the derivatives and analogs for treating cancer, reducing inflammation and/or treating an autoimmune or inflammatory disease.
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Paragraph 0972-0973
(2020/12/13)
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- IRAK DEGRADERS AND USES THEREOF
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The present invention provides compounds, compositions thereof, and methods of using the same.
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Paragraph 3617; 3618
(2019/07/10)
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- DERIVATIVES OF PIPERLONGUMINE AND USES THEREOF
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The present invention relates to a group of 1-[(E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]-2,3- dihydropyridin-6-one (piperlongumine) derivatives, analogs and pharmaceutically acceptable salts thereof. The present invention also relates to processes for preparing the same; a pharmaceutical composition and formulation containing a derivative of piperlogumine; and use of the derivatives and analogs for treating cancer.
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Page/Page column 227; 228
(2019/06/11)
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- BIS-BENZIMIDAZOLE COMPOUNDS AND METHODS OF USING SAME
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Provided herein are compounds and methods for modulating abnormal repeat expansions of gene sequences. More particularly, provided are inhibitors of RNA and the uses of such inhibitors in regulating nucleotide repeat expansions, e.g., to treat Myotonic Dystrophy Type 1 (DM1 ), Myotonic Dystrophy Type 2 (DM2), Fuchs dystrophy, Huntington Disease, Amyotrophic Lateral Sclerosis, or Frontotemporal Dementia.
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Paragraph 001031-001033
(2019/06/05)
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- HETEROCYCLIC COMPOUNDS CONTAINING AN INDOLE CORE
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Disclosed are novel compounds which inhibit RSK, methods of making such compounds and pharmaceutical compositions comprising such compounds. Also disclosed are methods of treating RSK2 regulated disorders using compounds of the invention.
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Page/Page column 91
(2011/06/26)
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- 3- (SULPHONYLAMINO) -PHENYL-2 -HYDROXY-ETHYLAMINO DERIVATIVES USEFUL AS BETA-AGONISTS, PROCESSES FOR PREPARING THEM AND THEIR USE AS MEDICAMENTS
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The present invention relates to compounds of general formula (I), wherein the groups A, L, R1 and R2 have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers, mixtures thereof, so
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Page/Page column 39
(2008/12/08)
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- Beta-agonists, methods for the preparation thereof and their use as pharmaceutical compositions
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The present invention relates to new beta-agonists of general formula (I) wherein the groups R1 to R4 have the meanings given in ths claims and specification, the tautomers, racemates, enantiomers, diastereomers, solvates, hydrates,
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Page/Page column 22
(2010/11/27)
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- Indol-containing beta-agonists, methods for the preparation thereof and their use as pharmaceutical compositions
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The present invention relates to new beta-agonists of general formula (I) wherein the groups R1 and R2 have the meanings given in the claims and specification, the tautomers, racemates, enantiomers, diastereomers, solvates, hydrates,
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Page/Page column 15
(2010/11/27)
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- Compounds with growth hormone releasing properties
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Disclosed are compounds of formula I formula I wherein R1, R2, R5, R6, R7, R8, G, J, L, M, a, b, c, d, e, and f are as defined in the specification, and compositions containing them. These
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- COMPOUNDS WITH GROWTH HORMONE RELEASING PROPERTIES
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This invention relates to novel compounds, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone.
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- Bicyclicpyrimidones and their use to treat diseases
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The present invention is directed to dihydropyrimidones having formula I or II and methods of using them to induce mitotic arrest, thereby making them useful as anti-cancer agents and other diseases that can be treated by inducing mitotic arrest.
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- Method for preparing a compound with growth hormone releasing properties
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A method for preparing a compound of formula I or a salt thereof is disclosed.
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- PYRROLOTRIAZINONE COMPOUNDS AND THEIR USE TO TREAT DISEASES
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The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts thereof useful for inducing mitotic arrest thereby making them useful as anti-cancer agents and other diseases which can be treated by inducing mitotic arrest.
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- Pyrrolotriazinone compounds and their use to teat diseases
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The present invention provides compounds of formula I and pharmaceutically acceptable salts thereof useful for inducing mitotic arrest thereby making them useful as anti-cancer agents and other diseases which can be treated by inducing mitotic arrest.
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- Compounds with growth hormone releasing properties
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This invention relates to novel compounds, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone.
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- Benzoamide piperidine containing compounds and related compounds
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The present invention relates to certain benzoamide piperidine containing compounds and related compounds that exhibit activity as NK-1 receptor antagonists, (e.g., substance P receptor antagonists), to pharmaceutical compositions containing them, and to their use in the treatment and prevention of central nervous system disorders, inflammatory disorders, cardiovascular disorders, ophthalmic disorders, gastrointestinal disorders, disorders caused by helicobacter pylori, disorders of the immune system, urinary incontinence, pain, migraine, emesis, angiogenesis and other disorders.
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- DPP IV inhibitors
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The present invention relates to compounds of formula (I) wherein R1, R2, and X are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV, such as diabetes, particularly non-insulin dependent diabetes mellitus, and impaired glucose tolerance.
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- COMPOUNDS WITH GROWTH HORMONE RELEASING PROPERTIES
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The present invention relates to novel compounds of general formula (I) which can be used for treating medical disorders resulting from a deficiency in growth hormone.
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- Use of growth hormone or a growth hormone secretagogue for promoting bone formation
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The invention provides a method of enhancing the healing of bone fractures in an animal subjected to distraction osteogenesis, the method comprising administering, to the animal in need thereof, a growth hormone or a growth hormone secretagogue in an amou
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- Compounds with growth hormone releasing properties
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The present invention relates to compounds, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone.
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Page column 58
(2010/02/06)
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- Compounds with growth hormone releasing properties
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There are disclosed novel synthetic peptides of the general formula (I) Compounds of formula (I) stimulate the release of growth hormone from the pituitary in humans and animals. A method for increasing the rate and extent of growth of animals to increase their milk and wool production or for the treatment of ailments, and the use of the compounds of formula (I) for the preparation of medicaments, are also disclosed.
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- Synthesis of N-protected 14C-labelled (2E)-5-amino-5-methylhex-2-enoic acid analogues
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A novel method of preparing N-protected (2E)-5-amino-5-methylhex-2-enoic acids has been developed based on the synthesis of 3-methyl-3-amino-butanol. The method was used to synthesise 14C-labelled compounds of (1) via synthesis of triethylphosphono[1-14C]acetate.
- Jessen, Claus U.,Selvig, Helle,Valsborg, Jacob S.
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p. 265 - 275
(2007/10/03)
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- Salt forms of (2E)-5-amino-5-methylhex-2-enoic acid N-methyl-N-((1R)-1-(N-methyl-N-((1R)-1-(methylcarbamoyl)-2-phenylethyl)carbamoyl)-2-(2-naphthyl)ethyl)amide
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The compounds disclosed are salts of (2E)-5-amino-5-methylhex-2-enoic acid N-methyl-N-((1R)-1-(N-methyl-N-((1R)-1-(methylcarbamoyl)-2-phenylethyl)carbamoyl)-2-(2-naphthyl)ethyl)amide of Formula I which have an aqueous solubility of at least 5 mg/ml, and a
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- Compounds with growth hormone releasing properties
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Compounds of the general formula I STR1 compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone are described.
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- Compounds with growth hormone releasing properties
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There are disclosed novel synthetic peptides of formula (I) where A, B, D, E, F, G, J, m, n, and p are defined in the specification. Compounds of formula (I) promote the release of growth hormone in humans and animals. Growth promoting compositions containing such compounds of formula (I) as the active ingredient, methods of stimulating the release of growth hormone, and the use of such compounds of formula (I) are also disclosed.
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- Compounds with growth hormone releasing properties
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Compounds of peptide mimetic nature having the general formula I STR1 wherein a and b are independently 1 or 2, R1 and R2 are independently H or C1-6 alkyl, G and J are independently, inter alia, aromats, and D and E are independently several different groups are growth hormone secretagogous with improved bioavailability.
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- Compounds with growth hormone releasing properties
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Novel peptide derivatives, compositions containing them, and their use for treating medical disorders resulting from a deficiency in growth hormone are disclosed. The peptides have the formula (I): STR1 wherein a, b, A, R1, L1, D, R3, R4, R2, L2, E and G are as defined in the specification. These peptides exhibit improved resistance to proteolytic degradation, and hence, improved bioavailability.
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- Compounds with growth hormone releasing properties
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The present invention relates to novel compounds of the general formula I STR1 which can be used for treating medical disorders resulting from a deficiency in growth hormone.
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- Novel orally active growth hormone secretagogues
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A novel class of growth hormone-releasing compounds with a molecular weight in the range from 500 to 650 has been discovered. The aim of this study was to obtain growth hormone secretagogues with oral bioavailability. By a rational approach we were able t
- Hansen, Thomas K.,Ankersen, Michael,Hansen, Birgit S.,Raun, Kirsten,Nielsen, Karin K.,Lau, Jesper,Peschke, Bernd,Lundt, Behrend F.,Th?gersen, Henning,Johansen, Nils L.,Madsen, Kjeld,Andersen, Peter H.
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p. 3705 - 3714
(2007/10/03)
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- Ornithine decarboxylase inhibiting branched aminooxy amino alkane derivatives
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Compounds of formula (I) in which (a) four of the radicals R1, R2, R3, R4, R5 and R6 are hydrogen and the others independently of one another are in each case C1 -C2 alkyl, these groups being bonded to the same carbon atom or to two different carbon atoms, or (b) five of the radicals R1, R2, R3, R4, R5 and R6 are hydrogen and the other radical is C1 -C2 alkyl or hydroxymethyl, or salts thereof, are described. The compounds of formula (I) and their salts are ornithine decarboxylase inhibitors.
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- Benzolactam growth hormone secretagogues: Replacement of the C-3 amide bond in L-692,429
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The synthesis and structure-activity relationships of various C-3 amide bond modifications in the novel nonpeptidyl growth hormone secretagogue L-692,429 are described. Several C-3 amide surrogates were prepared and the urea moiety was found to exhibit growth hormone releasing activity similar to that observed with L-692,429.
- Ok, Hyun O.,Szumiloski, John L.,Doldouras, George A.,Schoen, William R.,Cheng, Kang,Chan, Wanda W.-S.,Butler, Bridget S.,Smith, Roy G.,Fisher, Michael H.,Wyvratt, Matthew J.
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p. 3051 - 3056
(2007/10/03)
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